目的 研究粉防己碱(Tet)及5-溴粉防己碱(BrTet)在大鼠体内的代谢物。方法 大鼠分别ivTet及BrTet(20mg/kg)后采集尿液、粪便、胆汁和肝脏，用电喷雾离子阱多级质谱法(LC/MSⁿ)对Tet及BrTet在大鼠体内的代谢产物进行分析。结果 大鼠ivTet后，在体内可测到2个单去甲基、1个双去甲基、2个单羟化代谢物和2个氮氧化物；大鼠iv BrTet后，在体内可测到3个单去甲基、2个双去甲基、2个单羟化代谢物和2个氮氧化物，还测到脱溴代谢物(Tet)和进一步脱甲基代谢物，另外还测到4个相代谢物，分别是BrTet双去甲基硫酸结合物，单去甲基葡萄糖醛酸结合物，单羟化硫酸结合物和单羟化葡萄糖醛酸结合物。结论 Tet和BrTet在大鼠体内广泛代谢，二者具有相似的代谢途径，其代谢物的结构有待于进一步分析后确证。

Objective To investigate the metabolites of tetrandrine(Tet) and 5-bromo-tetrandrine(BrTet) in rat in vivo.Methods After rats were iv administered a single dose of Tet and BrTet(20 mg/kg),respectively,the samples of urine,feces,bile,and liver were collected.The metabolites of Tet and BrTet in rats in vivo were identified by LC/MCⁿ.Results After Tet was iv administered to rats,in addition to Tet itself,two nor-Tets,one di-nor-Tet,two hydro-Tet,and two Tet-N-oxides were found.After iv administration of BrTet to rats,a total of sixteen metabolites,including phase Ⅰ and phase Ⅱ metabolites,were found in rat bile.Phase Ⅰ metabolites were three nordemethyl-BrTets,two dinordemethyl-BrTets,Tet,two nor-Tets,two hydroxy-BrTets,and two Br Tets-N-oxides,respectively.Phase Ⅱ metabolites were di-nor-BrTets-sulfate,nor-BrTet-glucuronide,hydro-BrTet-sulfate,and hydro-BrTet-glucuronide,respectively.Conclusion Both Tet and BrTet are extensively metabolized and have similar metbolic pathways in rat.The structures of the metabolites will be further confirmed.

国家“973”项目(2004CB518902);天津重点基金项目(0YFJZJCO1101)